A Two-Step Synthesis of Unprotected 3-Aminoindoles via Post Functionalization with Nitrostyrene.

ABSTRACT: A novel, low-cost method for the preparation of not easily accessible free 3-aminoindoles has been developed. This approach is based on a well-established reaction between indoles and nitrostyrene in the presence of phosphorous acid, which results in the formation of 4'-phenyl-4'H-spiro[indole-3,5'-isoxazoles]. The latter could be transformed to corresponding aminated indoles by reaction with hydrazine hydrate in good or excellent yields upon microwave-assisted heating.

SUBMITTER: Aksenov NA 

PROVIDER: S-EPMC10180116 | biostudies-literature | 2023 Apr

REPOSITORIES: biostudies-literature